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Title 

CinQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo

Authors 

Dong Joon KimM H LeeK ReddyY LiD Y LimH XieS Y LeeYoung Il YeomA M BodeZ Dong

Publisher 

Oxford University Press (OUP)

Issue Date 

2013

Citation 

Carcinogenesis, vol. 34, no. 5, pp. 1134-1143

Abstract 

The mitogen-activated protein kinase kinase 1 and 2 signaling pathway is a major component of the RAS (Rat sarcoma)/RAF (Radpidly accelerated fibrosarcoma)/MEK (mitogen-activated protein kinase kinase)/ERKs (Extracellular signal-regulated kinases) signaling axis that regulates tumorigenesis and cancer cell growth. MEK is frequently activated in various cancers that have mutations in the KRAS and BRAF oncogenes. Therefore, MEK has been suggested as a therapeutic target for inhibitor development against tumors that are dependent on the activating mutations in mitogen-activated protein kinase signaling. Herein, we report the discovery of three novel MEK inhibitors, herein referred to as CInQ-01, CInQ-03 and CInQ-06. All three inhibitors were highly effective in suppressing MEK1 and MEK2 in vitro kinase activity as well as anchorage-dependent and anchorage-independent cell growth. The inhibitory activity was associated with markedly reduced phosphorylation of ERKs and ribosomal S6 kinases. Furthermore, administration of CInQ-03 inhibited colon cancer cell growth in an in vivo xenograft mouse model and showed no skin toxicity. Overall, these results suggest that these novel MEK inhibitors might be used for chemotherapy or prevention.

ISSN 

0143-3334

Link 

http://dx.doi.org/10.1093/carcin/bgt015

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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